5692-23-9Relevant academic research and scientific papers
Method for preparing derivatives of benzamide under microwave condition in aqueous phase
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Paragraph 0019; 0027, (2019/03/28)
The invention discloses a method for preparing derivatives of benzamide under a microwave condition in an aqueous phase. A coupling reaction is carried out between substituted benzoic acid and amine under the microwave condition in the aqueous phase. The method for preparing the derivatives of benzamide is environmentally friendly, easy and convenient to operate, safe, low in cost and efficient. Compared with the prior art, the method can be applicable to a large number of functional groups, is high in yield, produces fewer by-products, and further is easy to operate, safe, low in cost and environmentally friendly. A formula is shown in the description.
Cyclodehydration of N -(aminoalkyl)benzamides under mild conditions with a hendrickson reagent analogue
Loughlin, Wendy A.,Jenkins, Ian D.,Petersson, Maria J.
, p. 7356 - 7361 (2013/08/23)
Methods for the cyclodehydration of N-(aminoalkyl)benzamides are few and employ harsh reaction conditions. We have found that the easily prepared phosphonium anhydrides 1 (Hendrickson reagent) or 2 can be used for cyclodehydration of N-(aminoalkyl)benzamides under very mild conditions (room temperature) to produce five-, six-, and seven-membered cyclic amidines. Good yields are obtained by employing a temporary trityl group protection strategy. Cyclic analogue 2 can be used when the product cyclic amidine is organic-soluble, thus producing water-soluble byproducts.
Efficient and continuous monoacylation with superior selectivity of symmetrical diamines in microreactors
Maurya, Ram Awatar,Hoang, Phan Huy,Kim, Dong-Pyo
scheme or table, p. 65 - 68 (2012/03/26)
Efficient and continuous monoacylation of symmetrical diamines performed in microreactors yielded superior selectivity to that predicted by statistical considerations. It is highly valuable that the kinetically controlled product in high yields was achieved without any special catalyst at ambient temperature.
CDI-mediated monoacylation of symmetrical diamines and selective acylation of primary amines of unsymmetrical diamines
Verma, Sanjeev K.,Ghorpade, Ramarao,Pratap, Ajay,Kaushik
, p. 326 - 329 (2012/04/10)
A highly efficient and green protocol for monoacylation of symmetrical diamines and chemoselective acylation of primary amines of unsymmetrical diamines has been developed.
Structural analysis of ATP analogues compatible with kinase-catalyzed labeling
Suwal, Sujit,Senevirathne, Chamara,Garre, Satish,Pflum, Mary Kay H.
, p. 2386 - 2391 (2013/02/23)
Kinase-catalyzed protein phosphorylation is an important biochemical process involved in cellular functions. We recently discovered that kinases promiscuously accept γ-modified ATP analogues as cosubstrates and used several ATP analogues as tools for stud
New Potent Bisubstrate Inhibitors of Histone Acetyltransferase p300: Design, Synthesis and Biological Evaluation
Kwie, Franciane Ho A.,Briet, Martine,Soupaya, David,Hoffmann, Pascal,Maturano, Marie,Rodriguez, Frederic,Blonski, Casimir,Lherbet, Christian,Baudoin-Dehoux, Cecile
scheme or table, p. 86 - 92 (2011/09/15)
Bisubstrate-type compound Lys-CoA has been shown to inhibit the p300 histone acetyl transferase activity efficiently and may constitute a lead compound for a novel class of anticancer therapeutics. Based on this strategy, we synthesized a series of CoA derivatives and evaluated these molecules for their activity as p300 histone acetyltransferases inhibitor. The best activity was obtained with compound 3 bearing a C-5 spacing linker that connects the CoA moiety to a tert-butyloxycarbonyl (Boc) group. Based on docking simulations, this inhibitor exhibits favorable interactions with two binding areas, namely pockets P1 and P2, within the active site.
Imidazole-catalyzed monoacylation of symmetrical diamines
Verma, Sanjeev K.,Acharya,Kaushik
supporting information; experimental part, p. 4232 - 4235 (2010/11/04)
Figure Presented. An imidazole-catalyzed protocol for monoacylation of symmetrical diamines has been developed. The protocol gave selective monoacylation of aliphatic (cyclic and acyclic) primary and secondary diamines. In the reaction, imidazole acts as both catalyst and a leaving group. Different monoacylated piperazines and other diamines were synthesized at room temperature in an ethanol/water solvent system.
Phenyl esters, preferred reagents for mono-acylation of polyamines in the presence of water
Pappas, Kyrie,Zhang, Xiang,Tang, Wei,Fang, Shiyue
body text, p. 5741 - 5743 (2009/12/06)
In the presence of water, several diamines and one triamine were mono-acylated at ambient to moderate temperatures using phenyl esters and a phenyl carbonate as acylation agents in good to excellent isolated yields. Both linear and cyclic polyamines were suitable substrates, and the acylating agents can be aryl and alkyl carboxylic acid esters.
Mono-acylation of symmetric diamines in the presence of water
Tang, Wei,Fang, Shiyue
supporting information; scheme or table, p. 6003 - 6006 (2009/04/11)
Simply reacting equal equivalents of symmetric diamines with esters or carbonates in the presence of a suitable amount of water gave mono-acylated products in good to quantitative yields.
Selective Monoacylation of Symmetrical Diamines via Prior Complexation with Boron
Zhang, Zhongxing,Yin, Zhiwei,Meanwell, Nicholas A.,Kadow, John F.,Wang, Tao
, p. 3399 - 3402 (2007/10/03)
(Equation presented) Pretreatment of a symmetrical primary or secondary diamine with 9-BBN prior to the addition of an acyl chloride significantly suppressed undesired diacylation, and the product of monoacylation predominated. The reactive preference is interpreted as the result of a selective deactivation of one nitrogen atom of the diamine by 9-BBN.
